PSI-6130

PSI-6130
Clinical data
ATC code	none;
Identifiers
	IUPAC name 4-Amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyltetrahydrofuran-2-yl)pyrimidin-2(1H)-one;
CAS Number	817204-33-4 ;
PubChem CID	6481236;
ChemSpider	4981776;
UNII	05J68784G1;
ChEMBL	ChEMBL223482;
CompTox Dashboard (EPA)	DTXSID10231287 ;
Chemical and physical data
Formula	C10H14FN3O4
Molar mass	259.237 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@]1([C@@H]([C@H](O[C@H]1n2ccc(nc2=O)N)CO)O)F;
	InChI InChI=1S/C10H14FN3O4/c1-10(11)7(16)5(4-15)18-8(10)14-3-2-6(12)13-9(14)17/h2-3,5,7-8,15-16H,4H2,1H3,(H2,12,13,17)/t5-,7-,8-,10-/m1/s1; Key:NYPIRLYMDJMKGW-VPCXQMTMSA-N;
	(verify)

PSI-6130 is an experimental treatment for hepatitis C. PSI-6130 is a member of a class of antiviral drugs known as nucleoside polymerase inhibitors that was created by chemist Jeremy L. Clark.^[1] Specifically, PSI-6130 inhibits the hepatitis C virus RNA dependant RNA polymerase called NS5B.^[2]

PSI-6130 is currently being developed by Hoffmann–La Roche as a 3',5'-diisobutyrl ester prodrug, R7128.^[3] R7128 is part of the combination of all-oral agents clinical trial known as INFORM-1.^[4]

References

↑ Clark JL, Hollecker L, Mason JC, Stuyver LJ, Tharnish PM, Lostia S, et al. (August 2005). "Design, synthesis, and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methylcytidine, a potent inhibitor of hepatitis C virus replication". Journal of Medicinal Chemistry. 48 (17): 5504–8. doi:10.1021/jm0502788. PMID 16107149.
↑ Stuyver LJ, McBrayer TR, Tharnish PM, Clark J, Hollecker L, Lostia S, et al. (2006). "Inhibition of hepatitis C replicon RNA synthesis by beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine: a specific inhibitor of hepatitis C virus replication". Antiviral Chemistry & Chemotherapy. 17 (2): 79–87. doi:10.1177/095632020601700203. PMID 17042329. S2CID 22710780.
↑ Cole P, Castaner R, Bolos J (2009). "R-7128: RNA-directed RNA polymerase (NS5B) inhibitor treatment of hepatitis C virus infection". Drugs of the Future. 34 (4): 282–290. doi:10.1358/dof.2009.034.04.1367744.
↑ Gane EJ, Roberts SK, Stedman CA, Angus PW, Ritchie B, Elston R, et al. (October 2010). "Oral combination therapy with a nucleoside polymerase inhibitor (RG7128) and danoprevir for chronic hepatitis C genotype 1 infection (INFORM-1): a randomised, double-blind, placebo-controlled, dose-escalation trial". Lancet. 376 (9751): 1467–75. doi:10.1016/S0140-6736(10)61384-0. PMID 20951424. S2CID 28977802.

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[1] Clark JL, Hollecker L, Mason JC, Stuyver LJ, Tharnish PM, Lostia S, et al. (August 2005). "Design, synthesis, and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methylcytidine, a potent inhibitor of hepatitis C virus replication". Journal of Medicinal Chemistry. 48 (17): 5504–8. doi:10.1021/jm0502788. PMID 16107149.

[2] Stuyver LJ, McBrayer TR, Tharnish PM, Clark J, Hollecker L, Lostia S, et al. (2006). "Inhibition of hepatitis C replicon RNA synthesis by beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine: a specific inhibitor of hepatitis C virus replication". Antiviral Chemistry & Chemotherapy. 17 (2): 79–87. doi:10.1177/095632020601700203. PMID 17042329. S2CID 22710780.

[3] Cole P, Castaner R, Bolos J (2009). "R-7128: RNA-directed RNA polymerase (NS5B) inhibitor treatment of hepatitis C virus infection". Drugs of the Future. 34 (4): 282–290. doi:10.1358/dof.2009.034.04.1367744.

[4] Gane EJ, Roberts SK, Stedman CA, Angus PW, Ritchie B, Elston R, et al. (October 2010). "Oral combination therapy with a nucleoside polymerase inhibitor (RG7128) and danoprevir for chronic hepatitis C genotype 1 infection (INFORM-1): a randomised, double-blind, placebo-controlled, dose-escalation trial". Lancet. 376 (9751): 1467–75. doi:10.1016/S0140-6736(10)61384-0. PMID 20951424. S2CID 28977802.

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